Enhanced oral bioavailability and bioefficacy of phloretin using mixed polymeric modified self‐nanoemulsions

Abstract

Phloretin (Ph) is a natural active ingredient with wide biological properties. However, its poor water‐solubility and low oral bioavailability limit the application significantly in functional food and drug. This study was to explore the mixed polymer Pluronic® F127 and P123 modified the different triglycerides (LCT, MCT, SCT) in self‐nanoemulsions (SNEs) for enhancing the oral bioavailability and bioefficacy of Ph. The SNEs were characterized in terms of physical property study, lipolysis study, pharmacokinetic study, and anti‐inflammatory effect. The water‐solubility of LCT‐Ph‐SNE increased 3000‐fold compared with Ph solution. Pharmacokinetic study of SNEs and other carriers (HP‐β‐CD, PVP) results indicated that LCT‐Ph‐SNE was 7.9‐fold more bioavailable compared with unformulated Ph. The anti‐inflammatory activity of LCT‐Ph‐SNE in vivo represented a 6.8‐fold enhancement compared with unformulated Ph. This novel SNE formulation may also be used for other poorly soluble ingredients with high loading capacity, which made a significant impact on functional food and drug.

Role of Sodium-Glucose Co-Transporter 2 Inhibitors in the Regulation of Inflammatory Processes in Animal Models

“…Phlorizin was the first natural SGLT1/2 inhibitor discovered [ 8 ]. Despite its benefits improving insulin resistance [ 1 ] and diabetic complications such as nephropathy [ 23 ], non-alcoholic fatty liver disease [ 29 ], diabetic cardiomyopathy [ 35 ], or endothelial dysfunction [ 34 ], phlorizin had several drawbacks as a therapeutic agent, which included: (1) low oral bioavailability [ 60 ], (2) poor intestinal absorption and rapid clearance in urine [ 60 ], (3) low stability, being metabolized to phloretin in the small intestine by β-glucosidases [ 9 ], which inhibits GLUT1 [ 61 ] (responsible for glucose uptake in many tissues including the brain [ 62 ]), and (4) low solubility in water [ 63 ]. All of these observations, and the fact that mutations in the SGLT1 gene are associated with intestinal glucose–galactose malabsorption and associated fatal diarrhea [ 38 , 64 ], and that osmotic water flow through SGLT1 is blocked by phlorizin [ 65 ], prevented phlorizin from its use as an anti-diabetic drug.…”

The effects of nano‐zinc oxide morphology on functional and antibacterial properties of tapioca starch bionanocomposite

“…However, plastic waste is on the rise and is likely to reach more than 12,000 million metric tons by 2050 (Geyer et al., 2017 ). Therefore, the food packaging industry is trying to reduce the consumption of plastic polymers and replace them with renewable and natural biopolymers obtained from different sources (Wang et al., 2020 ; Zemljič et al., 2020 ). Various biopolymers such as lipids, polysaccharides, and proteins have been used for packaging purposes (Ekramian et al., 2021 ).…”

A Fungal Versatile GH10 Endoxylanase and Its Glycosynthase Variant: Synthesis of Xylooligosaccharides and Glycosides of Bioactive Phenolic Compounds

“…The yield of the main glycoside in each reaction relative to the initial acceptor concentration was also calculated from the HPLC chromatograms, achieving the highest values with hydroquinone (26.0%), gallic acid (21.7%), and rosmarinic acid (two major peaks of 20.9% and 20.0%, which represents a 40.9% acceptor conversion) (Table 3). However, it must be noted that in the case of phloretin and pterostilbene, some precipitation of the acceptor molecules was observed during the reactions due to their low solubility under the conditions tested [50,51], which could have caused an underestimation of glycoside yields. These results confirm that rXynSOS-E236G glycosynthase is a promising tool to glycosylate a broad range of phenolic compounds with biotechnological applications.…”